2361009-68-7

CAY10792 is an anticancer agent.¹ It binds to heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) in cell-free assays. CAY10792 inhibits the growth of A549, HCT116, U2OS, and MDA-MB-231 cancer cells (IC₅₀s = 0.54, 0.59, 0.57, and 0.57 μM, respectively) but not A549 cells overexpressing Hsp90, Cdc37, or Hsp90 and Cdc37 (IC₅₀s = >100 μM for all). It induces cell cycle arrest at the G₀/G₁ phase and apoptosis in A549 lung cancer cells when used at a concentration of 0.8 μM. In vivo, CAY10792 (0.5 and 1 mg/kg) reduces tumor weight in an A549 mouse xenograft model.

Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol?imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90?Cdc37 by covalent-binding, and induces apoptosis[1].

Hsp90-Cdc37

1. Li, N., Xu, M., Zhang, L., et al. Discovery of novel celastrol-imidazole derivatives with anticancer activity in vitro and in vivo J. Med. Chem. 65(6),4578-4589(2022).